Journal ArticleDOI
Applications of Fluorine in Medicinal Chemistry
TLDR
The effects of the strategic incorporation of fluorine in drug molecules and applications in positron emission tomography are provided, as well as new synthetic methodologies that allow more facile access to a wide range of fluorinated compounds.Abstract:
The role of fluorine in drug design and development is expanding rapidly as we learn more about the unique properties associated with this unusual element and how to deploy it with greater sophistication. The judicious introduction of fluorine into a molecule can productively influence conformation, pKa, intrinsic potency, membrane permeability, metabolic pathways, and pharmacokinetic properties. In addition, 18F has been established as a useful positron emitting isotope for use with in vivo imaging technology that potentially has extensive application in drug discovery and development, often limited only by convenient synthetic accessibility to labeled compounds. The wide ranging applications of fluorine in drug design are providing a strong stimulus for the development of new synthetic methodologies that allow more facile access to a wide range of fluorinated compounds. In this review, we provide an update on the effects of the strategic incorporation of fluorine in drug molecules and applications in po...read more
Citations
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Journal ArticleDOI
Next Generation of Fluorine-Containing Pharmaceuticals, Compounds Currently in Phase II–III Clinical Trials of Major Pharmaceutical Companies: New Structural Trends and Therapeutic Areas
Yu Zhou,Jiang Wang,Zhanni Gu,Shuni Wang,Wei Zhu,José Luis Aceña,Vadim A. Soloshonok,Kunisuke Izawa,Hong Liu +8 more
TL;DR: Compounds Currently in Phase II−III Clinical Trials of Major Pharmaceutical Companies: New Structural Trends and Therapeutic Areas is presented.
Journal ArticleDOI
3d Transition Metals for C-H Activation.
Parthasarathy Gandeepan,Thomas Müller,Daniel Zell,Gianpiero Cera,Svenja Warratz,Lutz Ackermann +5 more
TL;DR: A comprehensive overview on first row transition metal catalysts for C-H activation until summer 2018 is provided.
Journal ArticleDOI
Fluorine and Fluorinated Motifs in the Design and Application of Bioisosteres for Drug Design.
TL;DR: In this Perspective, applications of fluorine in the construction of bioisosteric elements designed to enhance the in vitro and in vivo properties of a molecule are summarized.
Journal ArticleDOI
Contribution of Organofluorine Compounds to Pharmaceuticals.
TL;DR: This mini-review analyzes the prevalence of fluoro-pharmaceuticals in the market and categorizes them into several groups based on the chemotype of thefluoro-functional groups, their therapeutic purpose, and the presence of heterocycles and/or chirality to highlight the structural motifs, patterns, and promising trends in fluorine-based drug design.
Journal ArticleDOI
Electrochemical strategies for C-H functionalization and C-N bond formation.
TL;DR: This review provides an overview on the use of anodic electrochemical methods for expediting the development of carbon-hydrogen functionalization and carbon-nitrogen bond formation strategies and aims to provide inspiration for future synthetic applications in the field of electrosynthesis.
References
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Journal ArticleDOI
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Journal ArticleDOI
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